title: Development of anti-EGF receptor peptidomimetics (AERP) as tumor imaging agent.
abstract: EGFR is over-expressed in several solid tumors including breast, prostate, pancreas, and lung cancers and is correlated to the metastatic potential of the tumor. Anti-EGFR receptor-binding peptidomimetics (AERP) were examined to assess the small molecule's potential use as tumor-specific imaging agents. The aim of this work was to design and characterize the binding specificity of the radiolabeled peptidomimetics to EGFR over-expressing cell lysate and to A431 xenograft tumors. Our newly designed peptidomimetic, AERP, was conjugated to DTPA and labeled with (99m)Tc. The in vivo tumor accumulation of [(99m)Tc] DTPA-AERP-2 was 1.6±0.1%ID/g and tumor to muscle ratio was 5.5. Our studies suggest that this novel peptidomimetic, AERP-2, warrants further development as an EGFR specific tumor-imaging agent.
authors.affiliation: Department of Radiology, Cyclotron Facility, 420 Curie Blvd., University of Pennsylvania, Philadelphia, PA 19104, United States. pondede@mail.med.upenn.edu
authors.forename: Datta E
authors.initials: DE
authors.lastname: Ponde
authors.forename: ZiFen
authors.initials: Z
authors.lastname: Su
authors.forename: Alan
authors.initials: A
authors.lastname: Berezov
authors.forename: Hongtao
authors.initials: H
authors.lastname: Zhang
authors.forename: Abbas
authors.initials: A
authors.lastname: Alavi
authors.forename: Mark I
authors.initials: MI
authors.lastname: Greene
authors.forename: Ramachandran
authors.initials: R
authors.lastname: Murali
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000000981:diagnostic imaging*; D004369:Pentetic Acid / Q000737:chemistry; D057786:Peptidomimetics; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry*; D013667:Technetium / Q000737:chemistry; D014018:Tissue Distribution; D014183:Transplantation, Heterologous
chemical_list: D004791:Enzyme Inhibitors; D057786:Peptidomimetics; D019275:Radiopharmaceuticals; D013667:Technetium; D004369:Pentetic Acid; D066246:ErbB Receptors